KR102290312B1 - Composition for tablet and preparing method thereof - Google Patents

Abstract

The tablet composition according to the present invention can be used universally by showing a fast oral disintegration rate and stable physical strength (hardness, friability) using only domestically acceptable food raw materials.

Description

Tablet composition and its preparation method {Composition for tablet and preparing method thereof}

The present invention relates to a tablet that rapidly dissolves in the oral cavity and a method for preparing the same.

In the case of the elderly, infants, people with difficulty in swallowing, and people who are physically or mentally difficult to manage due to dementia, it may be difficult to take tablets in a conventional way. In this regard, recently, a technology for preparing an oral fast-disintegrating tablet by various methods has been developed. Oral fast-disintegrating tablets disintegrate and dissolve rapidly in the oral cavity without water to form a solution or suspension and sequentially move to the absorption site of the digestive tract together with saliva. Therefore, it is possible to take without water for a wide range of age groups, such as those with dysphagia or the elderly and infants, thereby reducing the reluctance to take the tablet, and has the characteristics of allowing the active ingredient to be used quickly and sufficiently.

To date, various oral fast-disintegrating tablet manufacturing processes have been developed. A method of manufacturing a tablet by direct compression method by tableting, including a disintegrant, and a method of manufacturing a tablet by a special device and equipment without including a disintegrant. can be divided into

In the former case, sugar alcohols or sugars, disintegrants, excipients, and the like are obtained through direct compression using a tableting machine. From the group consisting of crospovidone, croscarmellose sodium and sodium starch glycolate to granulated and dried granules by mixing pharmaceutically acceptable salts and excipients as a representative prior patent technology A method for preparing a fast-disintegrating preparation (Patent Document 1) characterized in that it is lubricated and tableted through a step of post-mixing of one or more selected disintegrants and pharmaceutically acceptable additives and spray-dried mannitol, active Orally disintegrable tablet obtained by sieving and mixing ingredients, microcrystalline cellulose (average particle size 50 μm), croscarmellose sodium and lubricating agents such as magnesium stearate, and then directly compressing the final mixture (Patent Document 2) ), etc. However, representative disintegrants (carmellose, crospovidone, croscarmellose, sodium starch glycolate, etc.) presented in these patented technologies are not permitted as food additives in Korea, so they cannot be applied to food or health functional foods other than pharmaceuticals. There are limitations. Also, in most cases, other pharmaceutically usable raw materials are not food additives.

In the latter case, representative techniques include a freeze-drying method, a flash-tap method, a spray-drying method, and a supercritical fluid method. First, the most representative freeze-drying method is the Zydis method. This is a method of manufacturing tablets by filling a mold with a solution or suspension containing a drug and excipients, and then freeze-drying to remove the solvent. Since the prepared tablet has many micropores through which moisture escapes in its internal structure, it disintegrates and disperses within a few seconds when it comes into contact with a small amount of water. However, this technology requires expensive manufacturing equipment, takes a lot of time to manufacture, and has disadvantages in terms of hardness and friability of the finished product, so special packaging design is required. As a recent domestic patent related thereto, there is an oral formulation containing an active ingredient supported in the pores of a porous template by freeze-drying (Patent Document 3).

The flash tap method is a technology developed in Ethypharm, France. Using a solid dispersion technology, the drug particles were coated with a coating base, for example, Ammonio Methacrylate copolymer (Eudragit) to mask the bitter taste. , It is a tablet composed of micro-particles coated with appropriate excipients during the coating process.

The most representative method using the spray drying method is the WowTab technology of Yamanouchi of Japan. The method is characterized in that it is prepared by mixing low moldable saccharides and high moldable saccharides in an appropriate ratio, and then spray-drying them together with a drug. Patent Document 4 and Patent Document 5 are related to the technology of Wow Tap by a method using a spray drying method.

Finally, the supercritical fluid method is a technology for forming micropores by extracting a supercritical fluid soluble substance by tableting a mixture containing a supercritical fluid soluble material to obtain a tablet, and direct contact with the supercritical fluid soluble substance (Patent Document 6) ). It is true that the oral fast-disintegrating tablet technology manufactured without the use of a disintegrant is time and economically difficult to apply directly in the food or health functional food industry as it requires a large-scale investment in equipment or equipment.

As described above, although the manufacturing technology of the fast-disintegrating oral tablet is various, the oral fast-disintegrating tablet manufactured in common is designed to penetrate water more easily than a conventional formulation. These tablets disintegrate rapidly upon penetration of water and disperse and dissolve into small particles. In the case of an oral fast-disintegrating tablet, if the hardness is too low, the tablet is easily worn, whereas if the hardness is high, the disintegration time is delayed.

Republic of Korea Patent Publication No. 10-2014-0122017 Republic of Korea Patent Publication No. 10-2005-0062467 Republic of Korea Patent Publication No. 10-2014-0039354 US Patent Publication No. 5,576,014 US Patent No. 6,589,554 Republic of Korea Patent Publication No. 10-2010-0057390

It is an object of the present invention to provide a tablet composition that dissolves rapidly in the oral cavity. More specifically, it is to provide a tablet composition that can be used universally by using only raw materials permitted as food additives in Korea.

As a means for solving the above problems, the present invention

An oxidized starch comprising at least one selected from oxidized glucose represented by the following structural formulas 1 to 4 as a disintegrant,

Provided is a tablet composition comprising, as an excipient, at least one water-soluble sugar alcohol selected from the group consisting of erythritol, mannitol, xylitol, sorbitol and maltitol:

[Structural Formula 1]

[Structural Formula 2]

[Structural Formula 3]

[Structural Formula 4]

The tablet composition according to the present invention uses only food raw materials to prepare a tablet composition with high safety, fast disintegration time in the oral cavity, and improved physical strength such as friability and hardness.

1 is a graph showing that when oxidized starch is dispersed in water, there is little change in viscosity according to temperature change.
Figure 2 is a schematic representation of the action of the swelling agent (swelling agent) and wicking agent (wicking agent) in the tablet.
3 is a result showing the disintegration process of the tablet according to the present invention in purified water at 37 ℃ for each time period.

Hereinafter, the tablet composition of the present invention will be described in detail.

In the present invention, “tablet” refers to a solid preparation that is compressed with a tableting mixture containing conventional tablet components such as excipients, disintegrants, physiologically active substances, additives, lubricants, and the like, and the tablet according to the present invention is a food product. It may be an oral fast disintegrating tablet for use. The oral rapidly disintegrating tablet means a tablet designed to rapidly disintegrate in contact with saliva in the oral cavity without ingestion or mastication of water.

The present invention includes oxidized starch containing at least one selected from oxidized glucose represented by the following structural formulas 1 to 4 as a disintegrant, and erythritol, mannitol, xylitol, sorbitol as excipients ) and at least one water-soluble sugar alcohol selected from the group consisting of maltitol:

[Structural Formula 1]

[Structural Formula 2]

[Structural Formula 3]

[Structural Formula 4]

In the present invention, it may further include carboxymethylcellulose calcium and sucrose fatty acid ester as a disintegrant.

Oxidized starch is generally used as one of the modified starches used in the food industry for enhancing the crispness of fried products and for paper sizing in the paper industry, and is an unfamiliar ingredient for tableting.

In the oxidized starch of the present invention, starch chains are finely cut by treatment with an oxidizing agent, sodium hypochlorite, and carboxyl and carbonyl groups, which are hydrophilic residues, exist at the ends of the cut chains, so they are rapidly dispersed in water, as shown in FIG. 1 . It has the property of forming almost no viscosity. Thus, whereas starches generally act as a swelling agent by attracting moisture into the starch chains and increasing their volume when absorbing moisture in the tablet, oxidized starches have most of the chain particles cut off and hydrophilic residues. It is determined that the property of the wicking agent is more dominant (FIG. 2). This wicking action is observed to give a sustained and effective disintegration effect together with a sugar alcohol containing mannitol (FIG. 3).

In the present invention, the oxidized starch includes oxidized starch containing at least one oxidized glucose represented by the following structural formulas 1 to 4:

[Structural Formula 1]

[Structural Formula 2]

[Structural Formula 3]

[Structural Formula 4]

For example, the oxidized starch may be included in an amount of 5 to 40 wt%, preferably 10 to 30 wt%, and even more preferably 10 to 20 wt%, based on the total weight of the composition. By adjusting the content of the oxidized starch to the above range, it is possible to provide a tablet composition in which problems such as a characteristic odor and residual feeling in the oral cavity exhibited by the oxidized starch are improved.

In the present invention, the carboxymethyl cellulose calcium and sucrose fatty acid ester are used to promote the disintegration of the tablet. The carboxymethyl cellulose calcium is used to increase the contact area with moisture by helping the moisture to penetrate to the inside of the tablet by capillary action.

The sucrose fatty acid ester is used for accelerating dissolution of fat-soluble substances. As shown in FIG. 3 , when the tablet was put in purified water at 37° C., it was confirmed that some moisture rapidly moved into the tablet and cracked into large pieces. observed to contribute to disintegration.

Carboxymethyl cellulose calcium according to the present invention can be used by limiting it to 2% or less according to the standards and standards for each item in the National Food Additives Code. For example, the carboxymethylcellulose calcium may be included in an amount of 0.01 to 2% by weight, based on the total weight of the composition, and the sucrose fatty acid ester may be included in an amount of 0.01 to 1.5% by weight.

In the present invention, the disintegrant may include oxidized starch, carboxymethylcellulose calcium and sucrose fatty acid ester in a content ratio of 5 to 40: 0.01 to 2: 0.01 to 1.5.

In the present invention, the tablet composition includes an excipient together with the disintegrant.

The excipient may be a water-soluble sugar alcohol.

In the present invention, the water-soluble sugar alcohol includes at least one water-soluble sugar alcohol selected from the group consisting of erythritol, mannitol, xylitol, sorbitol and maltitol. When the water-soluble sugar alcohol is included in the composition of the present invention, it may exhibit the effect of assisting tablet disintegration and adding a refreshing feeling. In the present invention, the excipient may be mannitol.

For example, the excipient may be included in an amount of 50 to 85% by weight, preferably 60 to 80% by weight, and even more preferably 70 to 80% by weight based on the total weight of the composition.

In the present invention, the excipient and the oxidized starch are included in the composition in a content ratio of 50 to 85: 40 to 5, preferably 60 to 80: 30 to 10, and even more preferably 70 to 80: 20 to 10. can By adjusting the content ratio of the excipient and the oxidized starch to the above range, it is possible to provide a tablet having a short oral disintegration time and disintegration time, and stable hardness and friability.

The composition according to the present invention may further include additives in addition to the disintegrant and excipients.

In the present invention, the additive may be a food additive or an additive that is acceptable as a food that conforms to the standards and specifications of food additives of the Ministry of Food and Drug Safety in Korea.

The additive may include an auxiliary excipient for tablet tableting and stability enhancement, a lubricant for improving the fluidity of the composition to facilitate tableting, and a flavoring agent for improving the functionality of the formulation, such as flavoring agents, sweeteners and acidulants. However, the present invention is not limited thereto.

The auxiliary excipient may include crystalline cellulose, lactose and chicory extract powder, and the lubricant may include stearic acid, magnesium stearate, calcium stearate, polyethylene glycol and silicon dioxide, but polyethylene glycol and silicon dioxide have a health function It can be used only for food.

The flavoring agent may include berry flavor, lemon flavor, grape flavor, orange flavor, vanilla flavor, yogurt flavor, mint flavor, citrus flavor, apple flavor, chocolate flavor, etc. as a flavoring agent, but is not particularly limited as long as it is commonly used. . In addition, the sweetener may include at least one selected from the group consisting of aspartame, acesulfame K, sucralose, tomatine and stevia extract, and the acidulant may include malic acid, citric acid, lactic acid and tartaric acid, but is limited thereto it's not going to be

For example, the additive may be included in an amount of 0.02 to 40% by weight based on the total weight of the composition.

The composition of the present invention may further include a physiologically active substance. The physiologically active material may be one or more selected from the group consisting of raw materials and individually recognized health functional food raw materials that can be used according to standards and specifications of food or health functional food, and may include, for example, vitamins, minerals, probiotics, etc. , However, the present invention is not limited thereto. For example, the physiologically active substance may be vitamin B12.

In the present invention, the timing of addition of the physiologically active material is not limited, and may include both adding before granulation or separately post-addition after granulation.

The vitamin B12 may be included in an amount of 0.6 to 1.5 parts by weight based on 100 parts by weight of the total composition. By adjusting the content of vitamin B12 within the above range, it is possible to maintain a rapid oral disintegration rate, disintegration rate and formulation stability.

Therefore, the tablet composition according to the present invention can provide a tablet that rapidly dissolves in the oral cavity and exhibits rapid disintegration in the oral cavity, and the tablet can be used universally in food, particularly health functional food, by using an additive that is acceptable as food. .

The present invention provides a food composition comprising the composition.

The above foods include confectionery, chocolate, salt, soy sauce, complex seasoned food, processed sugar products, etc. according to the common standards and standards for general food of the National Food Code, and include all health functional foods in the ordinary sense. .

In the present invention, the term 'health functional food' refers to a food manufactured using raw materials or ingredients useful for the human body, and refers to a product focusing on a bioregulatory function that helps maintain and promote health. The food composition of the present invention can be prepared by a method commonly used in the art, and at the time of manufacture, it can be prepared by adding raw materials and components commonly added in the art.

The tablet composition of the present invention can be universally applied to various fields in which tablets are utilized, such as food, health functional food, pharmaceuticals, quasi-drugs and oral hygiene products.

In addition, the present invention provides a tablet comprising the composition.

Hereinafter, a method for preparing the tablet composition of the present invention will be described in detail.

The present invention provides a primary mixture by mixing at least one water-soluble sugar alcohol selected from the group consisting of erythritol, mannitol, xylitol, sorbitol and maltitol as an excipient and at least one selected from the group consisting of crystalline cellulose, lactose and chicory extract powder as an auxiliary excipient. preparing a;

preparing a secondary mixture by mixing oxidized starch containing at least one selected from oxidized glucose represented by the following structural formulas 1 to 4 as a disintegrant in the primary mixture, carboxymethylcellulose calcium, and sucrose fatty acid ester;

preparing a tertiary mixture by adding a flavoring agent and a physiologically active material to the secondary mixture; and

It provides a method for producing a tablet comprising the step of adding a lubricant to the tertiary mixture to lubricate and tabletting:

[Structural Formula 1]

[Structural Formula 2]

[Structural Formula 3]

[Structural Formula 4]

In the present invention, the first mixture may further include the step of preparing granules by adding a binding solution containing purified water to the mixture, kneading the mixture, sieving and drying the mixture.

In the manufacturing method of the tablet, disintegrants, excipients, auxiliary excipients, flavoring agents, physiologically active substances and lubricants can be applied or applied mutatis mutandis to all those described above, and the manufacturing method of the tablet is limited thereto. no. Any conventionally used tablet manufacturing method can be applied.

For example, the step of preparing the first mixture by mixing the excipient and the auxiliary excipient may include: mixing at least one water-soluble sugar alcohol selected as the excipient and the auxiliary excipient to obtain a first mixture for direct pressing; Alternatively, it may include all steps of obtaining granules by adding a binding solution containing purified water to the mixture, kneading the mixture, sieving with 20 mesh, and drying the mixture. In the present invention, the granulate may be dried so that a loss on drying (LOD) value of 1 to 3% in a dry oven at 50°C.

In addition, the step of preparing the secondary mixture includes the step of preparing a secondary mixture after mixing by adding a disintegrant to the primary mixture or granules prepared in the above step. The disintegrant may be mixed with oxidized starch, carboxymethylcellulose calcium and sucrose fatty acid ester in a content ratio of 5 to 40: 0.01 to 2: 0.01 to 1.5.

The preparing of the tertiary mixture includes preparing a tertiary mixture by mixing a flavoring agent and a physiologically active material with the secondary mixture. In the above step, the tertiary mixture may be prepared by uniformly post-mixing the antiseptic and the physiologically active material in the secondary mixture, but the timing of adding the physiologically active material is not limited thereto.

The method for manufacturing a tablet according to the present invention may further include a step of lubricating the prepared tertiary mixture by mixing a lubricant. In this step, the fluidity of the composition can be improved by lubricating the tertiary mixture.

In addition, the lubricated mixture may further include the step of tableting. Specifically, the step may include the step of preparing a compressed tablet by tableting the lubricated and improved fluidity composition. For example, the step of tableting the composition may be performed using a tableting method and a tableting machine commonly used in the art, for example, it may be performed using a single-shot tableting machine or a rotary (rotary) tableting machine.

In addition, the present invention provides a tablet prepared by the above manufacturing method.

The tablet according to the present invention can provide a tablet with high safety, fast disintegration time in the oral cavity, and improved physical strength such as hardness and friability.

Hereinafter, the present invention will be described in detail by the following examples. However, the following examples are merely illustrative of the present invention, and the content of the present invention is not limited to the following examples.

Example 1 to 10: tablet composition and tablet preparation

Tablet compositions and tablets were prepared according to the components and contents of Tables 1 to 4 below. In this case, tablet compositions and tablets were prepared by varying the types of water-soluble sugar alcohols (mannitol, sorbitol, erythritol, and xylitol) used as excipients and the ratio between water-soluble sugar alcohols and oxidized starch. Specifically, a first mixture was prepared by mixing water-soluble sugar alcohol and crystalline cellulose. The first mixture was mixed by adding oxidized starch, CMC calcium and sucrose fatty acid ester. Thereafter, a flavoring agent and a physiologically active substance were added as necessary, and magnesium stearate was added to lubricate the tablet, followed by tableting to prepare tablets.

[Ingredient used]

Oxidized starch (Samyang Genex Co., Ltd., Korea), mannitol (QINGDAO BRIGHT MOON SEAWEED GROUP Co., LTD., China), CMC calcium (BOLAK Co., Ltd., Korea), sucrose fatty acid ester (Mitsubishi-Kagaku) Foods Co., Japan), crystalline cellulose (MING TAI CHEMICAL Co., Ltd., Taiwan), and magnesium stearate (MALLINCKRODT INC., USA) are mixed compositions in the ratios described in Tables 1 to 4 below, using commercially available products. was prepared.

Experimental example 1: Characterization of tablets

The hardness, friability, oral disintegration time, and disintegration time of the tablets according to each Example prepared in Examples 1 to 9 were measured, and the results were statistically analyzed. The characteristic analysis method performed in this experimental example is as follows, and the results are shown in Tables 1 to 3 below.

[Hardness measurement]

The hardness of the tablet was measured using a hardness tester (Tablet Hardness Terter Model HT-50, Campbell Electronics, India), and 3 tablets were randomly collected and then measured and the average value was recorded.

[Measurement of Friability]

It was tested according to the method for measuring tablet friability described in Tablet Friability of the General chapters for general tests and analysis of USP (US Pharmacopoeia) 25.

[Oral disintegration test]

The disintegration test of fast-disintegrating tablets in the oral cavity was conducted by randomly selecting 5 people from among the panelists who had been engaged in sensory testing of food for more than 1 year. After the mouth was rinsed with purified water at 37° C., the time was measured by operating a stopwatch immediately after the tablets were placed on the tongues of the panelists. The panelists were prohibited from biting the tablet, and were allowed to gently roll the tablet within the limited space between the tongue and the roof of the mouth. This test was conducted after a sufficient adaptation process was performed in advance so that a similar time was obtained for the same test tablet. The stopwatch was immediately stopped at the time when disintegration of the tablet was completed together with saliva in the oral cavity and completely passed into the esophagus, and the time was recorded.

[Disintegration test]

It was tested according to the disintegration test method among the general test methods of health functional food standards and specifications (Ministry of Food and Drug Safety Notice No. 2016-143). Measurements were repeated three times, and all data were expressed as the average of the repeated experiment results.

[statistical analysis]

The results of the hardness measurement, oral disintegration test, and disintegration test repeated experiments were tested for significant difference using SAS program (version 9.4, SAS Institute Inc., Cary, N.C.), respectively (p<0.05).

Classification (content: wt%) Example 1 Example 2 Example 3 article
Castle
water
(%) mannitol 80 70 60 oxidized starch 10 20 30 CMC Calcium 2 2 2 sucrose fatty acid ester One One One crystalline cellulose 5 5 5 Magnesium Stearate 2 2 2 affection
my tabletting disorder does not exist does not exist does not exist Hardness (kp) 3.09 ± 0.03 ^A,B 3.23 ± 0.26 ^A,B 2.65 ± 0.15 ^B Friability (%) 0.43 0.39 0.49 Oral disintegration time (s) 25 ± 2 ^E,F 21 ± 2 ^F 20 ± 2 ^F Disintegration time (s) 57 ± 2 ^C 55 ± 3 ^C 89 ± 22 ^C

Classification (content: wt%) Example 4 Example 5 Example 6 article
Castle
water
(%) sorbitol 80 70 60 oxidized starch 10 20 30 CMC Calcium 2 2 2 sucrose fatty acid ester One One One crystalline cellulose 5 5 5 Magnesium Stearate 2 2 2 affection
my tabletting disorder does not exist does not exist does not exist Hardness (kp) 3.68 ± 0.76 ^A 3.55 ± 0.76 ^A 2.99 ± 0.39 ^A,B Friability (%) 0.13 0.19 0.14 Oral disintegration time (s) 61 ± 9 ^A,B 63 ± 21 ^A 54 ± 14 ^A,B,C Disintegration time (s) 225 ± 28 ^A,B 250 ± 23 ^A 239 ± 15 ^A,B

Classification (content: wt%) Example 7 Example 8 Example 9 article
Castle
water
(%) erythritol 80 70 60 oxidized starch 10 20 30 CMC Calcium 2 2 2 sucrose fatty acid ester One One One crystalline cellulose 5 5 5 Magnesium Stearate 2 2 2 affection
my tabletting disorder does not exist does not exist does not exist Hardness (kp) 3.33 ± 0.39 ^A,B 3.18 ± 0.04 ^A,B 3.05 ± 0.18 ^A,B Friability (%) 0.36 0.45 0.29 Oral disintegration time (s) 40 ± 13 ^C,D,E 34 ± 10 ^D,E,F 46 ± 8 ^B,C,D Disintegration time (s) 205 ± 37 ^B 253 ± 36 ^A 248 ± 5 ^A

(In Tables 1 to 3, A-F means that there is a significant difference at p<0.05 level when different superscripts are present in the same row.)

As shown in Tables 1 to 3, the tablet of Example 2 using mannitol as the water-soluble sugar alcohol and having a content ratio of mannitol and oxidized starch of 70:20 has the shortest oral disintegration time and disintegration time, and hardness and friability showed a reasonable level. Therefore, it was confirmed that applying the mannitol:oxidized starch content ratio of 70 to 80:10 to 20 corresponding to Examples 1 and 2 in consideration of the tablet test results and sensory matters showed the most excellent effect.

Example 10. Manufacture of tablets containing bioactive substances

Tablet compositions containing physiologically active substances were prepared according to the components and contents of Table 4 below. The content was expressed in two categories: the total content for all components and the rapidly disintegrating crystalline component in the oral cavity, and the functional and flavor component.

division ingredient total content
( parts by weight ) within the division content
( parts by weight ) Fast-disintegrating crystalline component in the oral cavity oxidized starch 14.81 15.00 CMC Calcium 1.97 2.00 sucrose fatty acid ester 0.99 1.00 mannitol 74.05 75.00 crystalline cellulose 4.9365 5.00 Magnesium Stearate 1.97 2.00 Functional
and
flavor ingredients vitamin B12 1.07 84.41 Enzyme-treated Stevia 0.15 11.69 malic acid 0.05 3.90

Experimental example 2. Comparative measurement with existing products

The tablets prepared in Example 10 were compared with existing products distributed abroad. The hardness, friability, oral disintegration time, and disintegration time of the tablet were measured by the same characteristic analysis method as in Experimental Example 1, and the results were analyzed statistically. The results are shown in Table 5 below. In Table 5 below, Comparative Example 1 used Solgar's trade name Sublingual Methylcobalamin, and the product was not added with a disintegrant. In Comparative Example 2, the trade name Vitamelts Energy of NatureMade was used, and the product used crospovidone as a disintegrant. Comparative Example 3 used the trade name Sublingual B-12 of Mason, and the product used croscamellose sodium as a disintegrant. Comparative Example 4 used Sundown's trade name Naturals Quick Dissolve Methylcobalamin, and the product used crospovidone as a disintegrant.

division Example 10 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Weight (mg) 140 130 330 180 110 Vitamin B12 /
Sokbung composition weight ratio 1.07 / 98.93 0.77 / 99.23 0.45 / 99.55 0.56 / 99.44 0.45 / 99.55 Prescription
(mg) Vitamin B12 1.5 One 1.5 One 0.5 break down
composition 138.5 129 328.5 179 109.5 Hardness (kp) 3.88 ± 0.41 ^A 1.48 ± 0.41 ^C 3.38 ± 0.25 ^A,B 1.09 ± 0.05 ^C 3.04 ± 0.69 ^B Friability (%) 0.29 1.17 0.57 0.50 0.18 Oral disintegration time (s) 28.20 ± 3.35 ^D 48.20 ± 11.17 ^B 43.20 ± 7.92 ^B,C 30.20 ±8.93 ^C,D 105.40± 14.47 ^A Disintegration time (s) 35.00 ± 4.00 ^C 39.67 ± 2.08 ^C 62.33 ± 2.52 ^B 56.67 ± 6.81 ^B 128.33± 15.01 ^A

(In Table 5, A-D means that there is a significant difference at the p<0.05 level when different superscripts are present in the same row.)

As shown in Table 5, it was found that the oral disintegration rate was the fastest in the case of the tablet of Example 10. As a result of statistical processing, Example 10 did not have a significant difference from Comparative Example 3, but in Comparative Example 3, the hardness was significantly low and the friability was high, so the tablet stability was relatively poor, and the disintegration time was also significantly slow can be seen.

In addition, it was found that Example 10 was the fastest in terms of disintegration time. As a result of statistical treatment, there was no significant difference from Comparative Example 1, but it felt as if it melted quickly because of the small tablet size of Comparative Example 1, and the oral disintegration time showed a significantly large difference, and the hardness was significantly low and the friability It was confirmed that the tablet stability was relatively poor.

In terms of hardness, it was found that Example 10 was the highest. Although there was no significant difference from Comparative Example 2, the oral disintegration rate and the disintegration rate were significantly faster, and the wear and tear was also found to be twice as stable.

Friability measurement results, Comparative Example 4 was the most dominant, but the oral disintegration time of Comparative Example 4 was slow enough to exceed 1 minute, and the disintegration time also exceeded 2 minutes, showing the lowest result among all Comparative Examples.

Considering these points comprehensively, Example 10 uses a disintegrant that cannot be used as a food additive in Korea, even though only food raw materials are used, and compared with existing products distributed abroad, which are known to have excellent oral disintegration effect. It was also found that it exhibited a high oral disintegration rate and stable physical strength (hardness, friability).

Claims (6)

Oxidized starch comprising at least one selected from oxidized glucose represented by the following structural formulas 1 to 4 as a disintegrant; and
Contains one or more water-soluble sugar alcohols selected from the group consisting of erythritol, mannitol, xylitol, sorbitol and maltitol as an excipient;
Provided that the oxidized starch is not included in the coating layer of the tablet, but a rapidly disintegrating oral tablet composition:
[Structural Formula 1]

[Structural Formula 2]

[Structural Formula 3]

[Structural Formula 4]

The method of claim 1,
The tablet composition is an oral fast disintegrating tablet composition, characterized in that it further comprises carboxymethylcellulose calcium (Carboxymethylcellulose Calcium, CMC calcium) and sucrose fatty acid ester as a disintegrant. The method of claim 1,
The tablet composition is an orally disintegrating tablet composition, characterized in that it comprises one or more additives selected from the group consisting of auxiliary excipients, lubricants and flavoring agents. The method of claim 1,
The tablet composition is an oral rapidly disintegrating tablet composition, characterized in that it further comprises a physiologically active substance. The method of claim 1,
The oxidized starch is an oral rapidly disintegrating tablet composition comprising 5 to 40% by weight relative to 100% by weight of the total tablet composition. 6. The method of claim 5,
The tablet composition is an orally disintegrating tablet composition comprising 50 to 85% by weight of a water-soluble sugar alcohol relative to 100% by weight of the total tablet composition.

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